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IDH-889

  Cat. No.:  DC10830   Featured
Chemical Structure
1429179-07-6
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More than 5000 active chemicals with high quality for research!
Field of application
IDH889 is a potent and selective inhibitors of IDH1. IDH899 shows IDH (R132H) IC50 = 20 nM; Cell 2-HG IC50 = 14 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1429179-07-6
Chemical Name: (4S)-3-[2-[[(1S)-1-[5-(4-Fluoro-3-methylphenyl)pyrimidin-2-yl]ethyl]amino]pyrimidin-4-yl]-4-propan-2-yl-1,3-oxazolidin-2-one
Synonyms: (4s)-3-[2-({(1s)-1-[5-(4-Fluoro-3-Methylphenyl)pyrimidin-2-Yl]ethyl}amino)pyrimidin-4-Yl]-4-(Propan-2-Yl)-1,3-Oxazolidin-2-One;7J2;(4S)-3-[2-[[(1S)-1-[5-(4-Fluoro-3-methylphenyl)pyrimidin-2-yl]ethyl]amino]pyrimidin-4-yl]-4-propan-2-yl-1,3-oxazolidin-2-one;IDH889
SMILES: FC1C([H])=C([H])C(=C([H])C=1C([H])([H])[H])C1C([H])=NC([C@]([H])(C([H])([H])[H])N([H])C2=NC([H])=C([H])C(=N2)N2C(=O)OC([H])([H])[C@]2([H])C([H])(C([H])([H])[H])C([H])([H])[H])=NC=1[H]
Formula: C23H25FN6O2
M.Wt: 436.4820
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM[1].
Target: IC50: 0.02 μM (IDH1R132H), 0.072 μM (IDH1R132C), 1.38 μM (IDH1wt)[1]
References: [1]. Levell JR, et al. Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1. ACS Med Chem Lett. 2016 Dec 16;8(2):151-156.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC7982 Mutant IDH1-IN-1 Mutant IDH1-IN-1 is a potent mutant IDH1 R132H inhibitor with IC50 < 0.1 uM(A level in Patent).
DC10830 IDH-889 IDH889 is a potent and selective inhibitors of IDH1. IDH899 shows IDH (R132H) IC50 = 20 nM; Cell 2-HG IC50 = 14 nM.
DC10538 IDH-305 IDH305 is an inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity.
DC7174 AGI-6780 AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q (IC50=23 nM).
DC5050 AGI-5198 AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.
DC10439 Vorasidenib (AG881) AG-881 is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1) in the cytoplasm and type 2 (IDH2).
DC8374 AG-221(Enasidenib) AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein.
DC8051 AG-120 (Ivosidenib) AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.
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